Related Experiment Video
Updated: Sep 16, 2025
16:36
Proteomics to Identify Proteins Interacting with P2X2 Ligand-Gated Cation Channels
Published on: May 18, 2009
14.8K
Radioligands Targeting the Purinergic P2X Receptors
Diego Dal Ben1, Michela Buccioni1, Catia Lambertucci1
1School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Via Madonna delle Carceri, I-62032 Camerino, Italy.
Cells
|July 11, 2025
Summary
Radioligands targeting Purinergic P2X receptors are crucial for disease research and diagnostics. While in vitro probes exist, in vivo imaging requires further development, though P2X7 antagonists show promise for brain PET scans.
Area of Science:
- Pharmacology
- Neuroscience
- Radiochemistry
Background:
- Purinergic P2X receptors are widely distributed and influence numerous physiological processes.
- These receptors are implicated in diseases including inflammation, neuroinflammation, neurodegeneration, and cancer.
- Developing specific radioligands for P2X receptor subtypes is vital for research and diagnostics.
Purpose of the Study:
- To review and summarize P2X receptor-targeting radioligands developed to date.
- To assess the suitability of these radioligands for in vitro and in vivo applications.
- To highlight advancements in radioligands for P2X receptor imaging.
Main Methods:
- Literature review of P2X receptor radioligands.
- Categorization of radioligands based on target P2X subtype and application (in vitro/in vivo).
- Analysis of radioligand characteristics, including affinity and selectivity.
Main Results:
- A range of radioligands targeting P2X receptors have been developed, from ATP analogues to allosteric modulators.
- Many high-affinity radioligands are suitable only for in vitro studies.
- No viable P2X3 or P2X4 radioligands for in vivo PET imaging have been reported.
- P2X7 antagonists ([11C]SMW139, [11C]GSK1482160, [11C]JNJ-54173717, [18F]JNJ-64413739) have been successfully used for brain PET imaging.
Conclusions:
- P2X receptor radioligands are essential tools for understanding disease mechanisms and developing therapeutics.
- Significant progress has been made in developing P2X-targeting radioligands, particularly for P2X7.
- Further research is needed to develop effective in vivo radioligands for P2X3 and P2X4 subtypes for broader diagnostic applications.
Keywords:
P2X receptorsPETimagingradioligandsradiotracerssingle-photon emission computed tomography (SPECT)More Related Videos
11:47Real-time Live-cell Flow Cytometry to Investigate Calcium Influx, Pore Formation, and Phagocytosis by P2X7 Receptors in Adult Neural Progenitor Cells
Published on: April 3, 2019
9.3K
08:33Measuring Nucleotide Binding to Intact, Functional Membrane Proteins in Real Time
Published on: March 11, 2021
2.1K
Related Concept Videos
01:31Transducer Mechanism: Nuclear Receptors
1.7K
Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
1.7K
01:12GPCR Desensitization
6.5K
G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
6.5K
01:15G Protein-coupled Receptors
13.5K
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
13.5K
01:30Ligand-Gated Ion Channel Receptor: Gating Mechanism
2.6K
Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
2.6K
01:27Transducer Mechanism: Enzyme-Linked Receptors
2.8K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Major types that are helpful drug targets include:
2.8K
01:09GPCRs Regulate Adenylyl Cylase Activity
6.0K
Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
6.0K